BMS-986202

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BMS-986202

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1771691-34-9

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

BMS-986202 是一种有效的，选择性的，具有口服活性的 Tyk2 抑制剂，可与 Tyk2 JH2 结合，IC50 为 0.19 nM，Ki 为 0.02 nM。BMS-986202 对包括 Jak 家族成员在内的其他激酶具有高度选择性。BMS-986202 还是 CYP2C19 的弱抑制剂，IC50 为 14 μM。BMS-986202 可用于 IL-23 驱动的棘皮症，抗 CD40 诱导的结肠炎和自发性狼疮的研究。

Cas No.	1771691-34-9
分子式	C₂₂H₁₈D₃FN₆O₃
分子量	439.46
溶解度	DMSO : 250 mg/mL (568.88 mM; Need ultrasonic)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research[1]. BMS-986202 inhibits IFNα and IL-23 in Kit225 T cells with IC50 values of 10 nM and 12 nM, respectively[1].BMS-986202 is potent in the IFNα stimulated STAT5 phosphorylation human whole blood (hWB) assay and mouse whole blood (mWB) with IC50 values of 58 nM and 481 nM, respectively[1]. BMS-986202 (Compound 7; 3-30 mg/kg; p.o.; daily; for 9 days) treatment inhibits IL-23-driven acanthosis in mice[1].BMS-986202 (Compound 7; 0.4-10 mg/kg; p.o.) treatment inhibits IL-12/IL-18-induced IFNγ production in mice. BMS-986202 dose-dependently inhibits IFNγ production by 46% and 80% at doses of 2 mg/kg and 10 mg/kg, respectively[1].BMS-986202 (Compound 7; 7-10 mg/kg; p.o.) is stable in liver microsomes, with half lives of greater than 120 min in mouse, rat, monkey, and humans and 89 min in dog. The serum protein binding for BMS-986202 in these species ranges from 89.3% to 96.0%, leaving a good range of free fraction of drug available. BMS-986202 shows the oral bioavailability up to 62-100%[1]. [1]. Chunjian Liu, et al. Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2. J Med Chem. 2021 Jan 14;64(1):677-694.